SPIO-Loaded Nanostructured Lipid Carriers for T2-weighted Magnetic Resonance Imaging of Hepatocarcinoma

Background The development of sensitive and specific MRI contrast agents for early diagnosis of hepatocellular carcinoma is highly demanded. Here, a peptide A54 (sequence: AGKGTPSLETTP) functionalized superparamagnetic iron oxide nanoparticles (SPIONs)-based magnetic nanostructured lipid carrier(A54-MNLC)as a hepatoma targeting negative magnetic resonance imaging (MRI) contrast agent was developed. Results Firstly, the A54 peptide functionalized PEGylated SA (A54-PEG-SA) was synthesized by the coupling reaction between A54 and NH2-PEG-SA. Then SPIONs-loaded MNLC(MNLC and A54-MNLC)were prepared by the solvent diffusion method. The A54-MNLC with a diameter of about 50 nm, and in vitro cell viability study revealed that the prepared A54-MNLC was cytocompatible in the given particles’ concentration ranges. The cellular uptake results indicated that A54-MNLC was able to be uptaken specifically by human hepatoma cell line (Bel-7402 cells) and also can be used as efficient probe for targeted MR imaging of cancer cells in vitro. The in vivo MR imaging experiments using an orthotopic implantation model further validated the hepatoma-targeting ability of A54-MNLC with a more remarkable MR imaging contrast effect compared to MNLC. Conclusions These results demonstrate that the A54-MNLC is a promising nanoplatform as a targeted MR imaging contrast agent for the diagnosis of hepatocellular carcinoma.